CA2866113C - Pyrazolyl derivatives as liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions - Google Patents

Pyrazolyl derivatives as liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions Download PDF

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Publication number
CA2866113C
CA2866113C CA2866113A CA2866113A CA2866113C CA 2866113 C CA2866113 C CA 2866113C CA 2866113 A CA2866113 A CA 2866113A CA 2866113 A CA2866113 A CA 2866113A CA 2866113 C CA2866113 C CA 2866113C
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CA
Canada
Prior art keywords
c6alkyl
aryl
pharmaceutically acceptable
compound
heteroaryl
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Expired - Fee Related
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CA2866113A
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English (en)
French (fr)
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CA2866113A1 (en
Inventor
Raju Mohan
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Ralexar Therapeutics Inc
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Ralexar Therapeutics Inc
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Publication of CA2866113A1 publication Critical patent/CA2866113A1/en
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Expired - Fee Related legal-status Critical Current
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/16Halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CA2866113A 2012-03-02 2013-02-28 Pyrazolyl derivatives as liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions Expired - Fee Related CA2866113C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261606160P 2012-03-02 2012-03-02
US61/606,160 2012-03-02
PCT/US2013/028438 WO2013130892A1 (en) 2012-03-02 2013-02-28 Liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions

Publications (2)

Publication Number Publication Date
CA2866113A1 CA2866113A1 (en) 2013-09-06
CA2866113C true CA2866113C (en) 2020-05-12

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CA2866113A Expired - Fee Related CA2866113C (en) 2012-03-02 2013-02-28 Pyrazolyl derivatives as liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions

Country Status (25)

Country Link
US (5) US8987318B2 (ko)
EP (2) EP2820013B9 (ko)
JP (2) JP6378630B2 (ko)
KR (1) KR102112879B1 (ko)
CN (1) CN104284893B (ko)
AU (1) AU2013225840B2 (ko)
BR (1) BR112014021515A2 (ko)
CA (1) CA2866113C (ko)
CY (1) CY1120742T1 (ko)
DK (1) DK2820013T3 (ko)
ES (1) ES2691079T3 (ko)
HK (1) HK1206030A1 (ko)
HR (1) HRP20181623T1 (ko)
HU (1) HUE040231T2 (ko)
IL (1) IL234413B (ko)
LT (1) LT2820013T (ko)
MX (1) MX361349B (ko)
NZ (1) NZ629636A (ko)
PL (1) PL2820013T3 (ko)
PT (1) PT2820013T (ko)
RS (1) RS57863B9 (ko)
SG (2) SG10201607345YA (ko)
SI (1) SI2820013T1 (ko)
TR (1) TR201815013T4 (ko)
WO (1) WO2013130892A1 (ko)

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Also Published As

Publication number Publication date
KR102112879B1 (ko) 2020-05-19
RS57863B9 (sr) 2019-10-31
CY1120742T1 (el) 2019-12-11
EP3441390A1 (en) 2019-02-13
EP2820013B9 (en) 2019-01-09
PT2820013T (pt) 2018-10-25
US20170334897A1 (en) 2017-11-23
DK2820013T3 (en) 2018-10-29
TR201815013T4 (tr) 2018-11-21
AU2013225840B2 (en) 2017-11-23
MX361349B (es) 2018-12-04
US20180370959A1 (en) 2018-12-27
BR112014021515A2 (pt) 2018-03-13
CN104284893B (zh) 2017-04-19
ES2691079T9 (es) 2019-02-08
US8987318B2 (en) 2015-03-24
PL2820013T3 (pl) 2019-01-31
ES2691079T3 (es) 2018-11-23
EP2820013A4 (en) 2015-11-11
HK1206030A1 (en) 2015-12-31
LT2820013T (lt) 2018-10-25
HUE040231T2 (hu) 2019-02-28
SI2820013T1 (sl) 2018-11-30
RS57863B1 (sr) 2018-12-31
CA2866113A1 (en) 2013-09-06
JP6378630B2 (ja) 2018-08-22
WO2013130892A1 (en) 2013-09-06
HRP20181623T1 (hr) 2018-12-14
US9637481B2 (en) 2017-05-02
SG10201607345YA (en) 2016-11-29
JP2018184467A (ja) 2018-11-22
JP2015512883A (ja) 2015-04-30
KR20140146089A (ko) 2014-12-24
SG11201405378VA (en) 2014-09-26
JP6800922B2 (ja) 2020-12-16
US20150045399A1 (en) 2015-02-12
CN104284893A (zh) 2015-01-14
EP2820013B1 (en) 2018-07-11
AU2013225840A1 (en) 2014-09-18
IL234413B (en) 2018-05-31
EP2820013A1 (en) 2015-01-07
NZ629636A (en) 2017-02-24
US20150152094A1 (en) 2015-06-04
MX2014010537A (es) 2015-03-09
US20210101895A1 (en) 2021-04-08

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